HRP20180916T1 - Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use - Google Patents

Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use Download PDF

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Publication number
HRP20180916T1
HRP20180916T1 HRP20180916TT HRP20180916T HRP20180916T1 HR P20180916 T1 HRP20180916 T1 HR P20180916T1 HR P20180916T T HRP20180916T T HR P20180916TT HR P20180916 T HRP20180916 T HR P20180916T HR P20180916 T1 HRP20180916 T1 HR P20180916T1
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HR
Croatia
Prior art keywords
compound
phenyl
trans
compound according
cyclopropylamino
Prior art date
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HRP20180916TT
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Croatian (hr)
Inventor
Alberto ORTEGA MUÑOZ
Matthew Colin Thor Fyfe
Marc Martinell Pedemonte
Iñigo TIRAPU FERNANDEZ DE LA CUESTA
Maria de los Ángeles ESTIARTE-MARTÍNEZ
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Oryzon Genomics, S.A.
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Application filed by Oryzon Genomics, S.A. filed Critical Oryzon Genomics, S.A.
Publication of HRP20180916T1 publication Critical patent/HRP20180916T1/en

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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Claims (29)

1. Spoj, naznačen time, da ima Formulu (I) ili njegova farmaceutski prihvatljiva sol ili njegov solvat: u kojoj: (A) je aril-skupina ili heteroaril-skupina, pri čemu navedena aril-skupina ili navedena heteroaril-skupina ima n supstituenata (R3); (B) je –O-CH2-fenil ili fenil, pri čemu navedeni fenil ili dio molekule fenila obuhvaćen u navedenom –O-CH2-fenilu, ima n supstituenata (R2); (D) je monociklička heteroaril-skupina, pri čemu navedena heteroaril-skupina ima jedan supstituent (R1), i nadalje time, da je navedena heteroaril-skupina kovalentno vezana na ostatak molekule preko prstenskog atoma ugljika; (R1) je –NH2; svaki (R2) je neovisno odabran od sljedećih: alkil, alkenil, alkinil, ciklil, amino, amido, C-amido, alkilamino, hidroksil, nitro, halo, haloalkil, haloalkoksi, cijano, sulfinil, sulfonil, sulfonamid, alkoksi, acil, karboksil, karbamat ili urea; svaki (R3) je neovisno odabran od sljedećih: alkil, alkenil, alkinil, ciklil, amino, amido, C-amido, alkilamino, hidroksil, nitro, halo, haloalkil, haloalkoksi, cijano, sulfinil, sulfonil, sulfonamid, alkoksi, acil, karboksil, karbamat ili urea; i n je neovisno 0, 1, 2, 3, ili 4.1. A compound of Formula (I) or a pharmaceutically acceptable salt or solvate thereof: where: (A) is an aryl group or a heteroaryl group, wherein said aryl group or said heteroaryl group has n substituents (R3); (B) is –O-CH2-phenyl or phenyl, wherein said phenyl or part of the phenyl molecule included in said –O-CH2-phenyl has n substituents (R2); (D) is a monocyclic heteroaryl group, wherein said heteroaryl group has one substituent (R1), and furthermore, that said heteroaryl group is covalently bound to the rest of the molecule via a ring carbon atom; (R 1 ) is –NH 2 ; each (R 2 ) is independently selected from the following: alkyl, alkenyl, alkynyl, cyclyl, amino, amido, C-amido, alkylamino, hydroxyl, nitro, halo, haloalkyl, haloalkoxy, cyano, sulfinyl, sulfonyl, sulfonamide, alkoxy, acyl, carboxyl, carbamate or urea; each (R 3 ) is independently selected from the following: alkyl, alkenyl, alkynyl, cyclyl, amino, amido, C-amido, alkylamino, hydroxyl, nitro, halo, haloalkyl, haloalkoxy, cyano, sulfinyl, sulfonyl, sulfonamide, alkoxy, acyl, carboxyl, carbamate or urea; and n is independently 0, 1, 2, 3, or 4. 2. Spoj prema zahtjevu 1, naznačen time, da (A) je fenil, piridinil, tiofenil, pirolil, furanil, ili tiazolil, i nadalje time, da (A) ima n supstituenata (R3).2. A compound according to claim 1, characterized in that (A) is phenyl, pyridinyl, thiophenyl, pyrrolyl, furanyl, or thiazolyl, and further in that (A) has n substituents (R3). 3. Spoj prema zahtjevu 1, naznačen time, da (A) je fenil ili piridil, i nadalje time, da navedeni fenil ili navedeni piridil ima n supstituenata (R3).3. A compound according to claim 1, characterized in that (A) is phenyl or pyridyl, and further in that said phenyl or said pyridyl has n substituents (R3). 4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time, da (A) ima n supstituenata (R3).4. A compound according to any one of claims 1 to 3, characterized in that (A) has n substituents (R3). 5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time, da (B) ima 0 ili 1 supstituent (R2).5. A compound according to any one of claims 1 to 4, characterized in that (B) has 0 or 1 substituent (R2). 6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da (D) je tiazolil, oksadiazolil, oksazolil, izoksazolil, tiadiazolil, triazinil, piridazinil, pirazinil, piridinil, ili pirimidinil, i nadalje time, da navedeni tiazolil, navedeni oksadiazolil, navedeni oksazolil, navedeni izoksazolil, navedeni tiadiazolil, navedenitriazinil, navedeni piridazinil, navedeni pirazinil, navedeni piridinil, ili navedeni pirimidinil ima jedan supstituent (R1).6. A compound according to any one of claims 1 to 5, characterized in that (D) is thiazolyl, oxadiazolyl, oxazolyl, isoxazolyl, thiadiazolyl, triazinyl, pyridazinyl, pyrazinyl, pyridinyl, or pyrimidinyl, and further in that said thiazolyl, said oxadiazolyl, said oxazolyl, said isoxazolyl, said thiadiazolyl, said triazinyl, said pyridazinyl, said pyrazinyl, said pyridinyl, or said pyrimidinyl has one substituent (R1). 7. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time, da (D) je oksadiazolil, pri čemu navedeni oksadiazolil ima jedan supstituent (R1).7. A compound according to any one of claims 1 to 6, characterized in that (D) is oxadiazolyl, wherein said oxadiazolyl has one substituent (R1). 8. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time, da (R2) je neovisno odabran od hidroksila, halo ili haloalkila.8. A compound according to any one of claims 1 to 7, characterized in that (R 2 ) is independently selected from hydroxyl, halo or haloalkyl. 9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time, da su supstituenti na dijelu molekule ciklopropila u trans-konfiguraciji.9. A compound according to any one of claims 1 to 8, characterized in that the substituents on the part of the cyclopropyl molecule are in the trans-configuration. 10. Spoj prema zahtjevu 1, naznačen time, da je navedeni spoj odabran od sljedećih: 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)pirimidin-2-amin; 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)tiazol-2-amin; 5-(((trans)-2-(6-(3-trifluorometil)fenil)piridin-3-il)ciklopropilamino)metil)pirimidin-2-amin; 5-(((trans)-2-(6-(3-trifluorometil)fenil)piridin-3-il)ciklopropilamino)metil)tiazol-2-amin; 3-(5-((trans)-2-((2-aminopirimidin-5-il)metilamino)ciklopropil)piridin-2-il)fenol; 3-(5-((trans)-2-((2-aminotiazol-5-il)metilamino)ciklopropil)piridin-2-il)fenol; 4'-((trans)-2-((2-aminopirimidin-5-il)metilamino)ciklopropil)bifenil-3-ol; 4'-((trans)-2-((2-aminotiazol-5-il)metilamino)ciklopropil)bifenil-3-ol; 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,2,4-oksadiazol-3-amin; 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.10. Compound according to claim 1, characterized in that said compound is selected from the following: 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)pyrimidin-2-amine; 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)thiazol-2-amine; 5-(((trans)-2-(6-(3-trifluoromethyl)phenyl)pyridin-3-yl)cyclopropylamino)methyl)pyrimidin-2-amine; 5-(((trans)-2-(6-(3-trifluoromethyl)phenyl)pyridin-3-yl)cyclopropylamino)methyl)thiazol-2-amine; 3-(5-((trans)-2-((2-aminopyrimidin-5-yl)methylamino)cyclopropyl)pyridin-2-yl)phenol; 3-(5-((trans)-2-((2-aminothiazol-5-yl)methylamino)cyclopropyl)pyridin-2-yl)phenol; 4'-((trans)-2-((2-aminopyrimidin-5-yl)methylamino)cyclopropyl)biphenyl-3-ol; 4'-((trans)-2-((2-aminothiazol-5-yl)methylamino)cyclopropyl)biphenyl-3-ol; 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)-1,2,4-oxadiazol-3-amine; 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)-1,3,4-oxadiazol-2-amine; or a pharmaceutically acceptable salt or solvate thereof. 11. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je: 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.11. Compound according to claim 1, characterized in that said compound is: 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)-1,3,4-oxadiazol-2-amine; or a pharmaceutically acceptable salt or solvate thereof. 12. Spoj prema bilo kojem od zahtjeva 9 do 11, naznačen time, da navedeni spoj je optički aktivan stereoizomer.12. A compound according to any one of claims 9 to 11, characterized in that said compound is an optically active stereoisomer. 13. Spoj prema bilo kojem od zahtjeva 9 do 12, naznačen time, da navedeni spoj je (-) stereoizomer.13. A compound according to any one of claims 9 to 12, characterized in that said compound is (-) stereoisomer. 14. Spoj prema bilo kojem od zahtjeva 9 do 12, naznačen time, da navedeni spoj je (+) stereoizomer.14. A compound according to any one of claims 9 to 12, characterized in that said compound is a (+) stereoisomer. 15. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je: (-) 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.15. Compound according to claim 1, characterized in that said compound is: (-) 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)-1,3,4-oxadiazol-2-amine; or a pharmaceutically acceptable salt or solvate thereof. 16. Farmaceutski pripravak, naznačen time, da on obuhvaća spoj prema bilo kojem od zahtjeva 1 do 15 i farmaceutski prihvatljiv nosač.16. A pharmaceutical preparation, characterized in that it comprises a compound according to any one of claims 1 to 15 and a pharmaceutically acceptable carrier. 17. Spoj prema bilo kojem od zahtjeva 1 do 15, ili farmaceutski pripravak prema zahtjevu 16, naznačen time, da se upotrebljava kao lijek.17. A compound according to any one of claims 1 to 15, or a pharmaceutical preparation according to claim 16, characterized in that it is used as a medicine. 18. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji neurološke bolesti ili neurološkog poremećaja.18. A compound according to any one of claims 1 to 15, characterized in that it is used in the treatment or prevention of a neurological disease or neurological disorder. 19. Spoj za uporabu prema zahtjevu 18, naznačen time, da navedeni spoj je: 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.19. Compound for use according to claim 18, characterized in that said compound is: 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)-1,3,4-oxadiazol-2-amine; or a pharmaceutically acceptable salt or solvate thereof. 20. Spoj za uporabu prema zahtjevu 18, naznačen time, da navedeni spoj je: (-) 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.20. Compound for use according to claim 18, characterized in that said compound is: (-) 5-(((trans)-2-(4-(benzyloxy)phenyl)cyclopropylamino)methyl)-1,3,4-oxadiazol-2-amine; or a pharmaceutically acceptable salt or solvate thereof. 21. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 20, naznačen time, da je navedena neurološka bolest ili navedeni neurološki poremećaj odabrana/odabran od sljedećih: depresija, Alzheimerova bolest, Huntingtonova bolest, Parkinsonova bolest, amiotrofna lateralna skleroza, frontotemporalna demencija ili demencija s Lewy tijelima.21. A compound for use according to any one of claims 18 to 20, characterized in that is said neurological disease or said neurological disorder selected from the following: depression, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, frontotemporal dementia or dementia with Lewy bodies. 22. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Alzheimerova bolest.22. The compound for use according to any one of claims 18 to 21, characterized in that said neurological disease or said neurological disorder is Alzheimer's disease. 23. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Huntingtonova bolest.23. The compound for use according to any one of claims 18 to 21, characterized in that said neurological disease or said neurological disorder is Huntington's disease. 24. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Parkinsonova bolest.24. The compound for use according to any one of claims 18 to 21, characterized in that said neurological disease or said neurological disorder is Parkinson's disease. 25. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je amiotrofna lateralna skleroza.25. The compound for use according to any one of claims 18 to 21, characterized in that said neurological disease or said neurological disorder is amyotrophic lateral sclerosis. 26. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji raka.26. A compound according to any one of claims 1 to 15, characterized in that it is used in the treatment or prevention of cancer. 27. Spoj za uporabu prema zahtjevu 26, naznačen time, da je navedeni rak odabran od sljedećih: rak prostate, rak dojke, rak pluća, kolorektalni rak, rak mozga, rak kože, rak krvi, leukemija, limfom, ili mijelom.27. The compound for use according to claim 26, characterized in that said cancer is selected from the following: prostate cancer, breast cancer, lung cancer, colorectal cancer, brain cancer, skin cancer, blood cancer, leukemia, lymphoma, or myeloma. 28. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji virusne infekcije.28. A compound according to any one of claims 1 to 15, characterized in that it is used in the treatment or prevention of a viral infection. 29. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji virusne reaktivacije nakon latentnog stanja. 29. A compound according to any one of claims 1 to 15, characterized in that it is used in the treatment or prevention of viral reactivation after a latent state.
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